4QQJ
 
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4QQT
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4CLJ
 | | Structure of L1196M Mutant Human Anaplastic Lymphoma Kinase in Complex with PF-06463922 ((10R)-7-amino-12-fluoro-2,10,16-trimethyl- 15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo(4,3-h)(2,5,11) benzoxadiazacyclotetradecine-3-carbonitrile). | | Descriptor: | (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile, ALK TYROSINE KINASE RECEPTOR | | Authors: | McTigue, M.A, Deng, Y.L, Liu, W, Brooun, A, Stewart, A.E. | | Deposit date: | 2014-01-14 | | Release date: | 2014-05-28 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (1.66 Å) | | Cite: | Discovery of (10R)-7-Amino-12-Fluoro-2,10,16-Trimethyl-15-Oxo-10,15,16,17-Tetrahydro-2H-8,4-(Metheno)Pyrazolo[4,3-H][2,5,11]Benzoxadiazacyclotetradecine-3-Carbonitrile (Pf-06463922), a Macrocyclic Inhibitor of Alk/Ros1 with Pre-Clinical Brain Exposure and Broad Spectrum Potency Against Alk-Resistant Mutations.
J.Med.Chem., 57, 2014
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4QRC
 | | Crystal Structure of the Tyrosine Kinase Domain of FGF Receptor 4 in Complex with Ponatinib | | Descriptor: | 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzam ide, Fibroblast growth factor receptor 4, SULFATE ION | | Authors: | Huang, Z, Mohammadi, M. | | Deposit date: | 2014-06-30 | | Release date: | 2014-10-29 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (1.901 Å) | | Cite: | DFG-out Mode of Inhibition by an Irreversible Type-1 Inhibitor Capable of Overcoming Gate-Keeper Mutations in FGF Receptors.
Acs Chem.Biol., 10, 2015
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4E20
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4DFL
 | | Crystal structure of spleen tyrosine kinase complexed with a sulfonamidopyrazine piperidine inhibitor | | Descriptor: | 1,2-ETHANEDIOL, 3-amino-6-{3-[(methylsulfonyl)amino]phenyl}-N-(piperidin-4-ylmethyl)pyrazine-2-carboxamide, SULFATE ION, ... | | Authors: | Lopez, M, Segarra, V, Vidal, B, Wenzkowski, C, Jestel, A, Krapp, S, Blaesse, M, Nagel, S, Schreiner, P. | | Deposit date: | 2012-01-24 | | Release date: | 2012-04-25 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (1.98 Å) | | Cite: | Pyrazine-based Syk kinase inhibitors.
Bioorg.Med.Chem.Lett., 22, 2012
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3CTH
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4R6V
 | | Crystal Structure of FGF Receptor (FGFR) 4 Kinase Harboring the V550L Gate-Keeper Mutation in Complex with FIIN-3, an Irreversible Tyrosine Kinase Inhibitor Capable of Overcoming FGFR kinase Gate-Keeper Mutations | | Descriptor: | Fibroblast growth factor receptor 4, N-[4-({[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](6-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)amino}methyl)phenyl]propanamide, SULFATE ION | | Authors: | Huang, Z, Mohammadi, M. | | Deposit date: | 2014-08-26 | | Release date: | 2014-10-29 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.353 Å) | | Cite: | Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.
Proc.Natl.Acad.Sci.USA, 111, 2014
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3D7T
 | | Structural basis for the recognition of c-Src by its inactivator Csk | | Descriptor: | Proto-oncogene tyrosine-protein kinase Src, STAUROSPORINE, Tyrosine-protein kinase CSK | | Authors: | Levinson, N.M, Seeliger, M.A, Cole, P.A, Kuriyan, J. | | Deposit date: | 2008-05-21 | | Release date: | 2008-08-05 | | Last modified: | 2021-10-20 | | Method: | X-RAY DIFFRACTION (2.899 Å) | | Cite: | Structural basis for the recognition of c-Src by its inactivator Csk.
Cell(Cambridge,Mass.), 134, 2008
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4ZSA
 | | Crystal structure of FGFR1 kinase domain in complex with 7n | | Descriptor: | 4-(4-ethylpiperazin-1-yl)-N-[6-(3-methoxyphenyl)-2H-indazol-3-yl]benzamide, Fibroblast growth factor receptor 1 | | Authors: | Liu, Q.F, Xu, Y.C. | | Deposit date: | 2015-05-13 | | Release date: | 2015-06-17 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Design, synthesis and biological evaluation of novel FGFR inhibitors bearing an indazole scaffold.
Org.Biomol.Chem., 13, 2015
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3D4Q
 | | Pyrazole-based inhibitors of B-Raf kinase | | Descriptor: | (1E)-5-(1-piperidin-4-yl-3-pyridin-4-yl-1H-pyrazol-4-yl)-2,3-dihydro-1H-inden-1-one oxime, B-Raf proto-oncogene serine/threonine-protein kinase | | Authors: | Morales, T, Vigers, G.P.A, Brandhuber, B.J. | | Deposit date: | 2008-05-14 | | Release date: | 2008-08-19 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Potent and selective pyrazole-based inhibitors of B-Raf kinase.
Bioorg.Med.Chem.Lett., 18, 2008
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3D7U
 | | Structural basis for the recognition of c-Src by its inactivator Csk | | Descriptor: | Proto-oncogene tyrosine-protein kinase Src, Tyrosine-protein kinase CSK | | Authors: | Levinson, N.M, Seeliger, M.A, Cole, P.A, Kuriyan, J. | | Deposit date: | 2008-05-21 | | Release date: | 2008-08-05 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (4.111 Å) | | Cite: | Structural basis for the recognition of c-Src by its inactivator Csk.
Cell(Cambridge,Mass.), 134, 2008
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4R7H
 | | Crystal structure of FMS KINASE domain with a small molecular inhibitor, PLX3397 | | Descriptor: | 5-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-N-{[6-(trifluoromethyl)pyridin-3-yl]methyl}pyridin-2-amine, Macrophage colony-stimulating factor 1 receptor | | Authors: | Zhang, Y, Zhang, K, Zhang, C. | | Deposit date: | 2014-08-27 | | Release date: | 2015-08-12 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.8001 Å) | | Cite: | Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor.
N Engl J Med, 373, 2015
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4RG0
 | | Crystal structure of BTK kinase domain complexed with 2-[8-fluoro-2-[2-(hydroxymethyl)-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)-2-pyridyl]amino]-6-oxo-3-pyridyl]phenyl]-1-oxo-3,4-dihydroisoquinolin-6-yl]-2-methyl-propanenitrile | | Descriptor: | 2-{8-fluoro-2-[2-(hydroxymethyl)-3-(1-methyl-5-{[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino}-6-oxo-1,6-dihydropyridin-3-yl)phenyl]-1-oxo-1,2,3,4-tetrahydroisoquinolin-6-yl}-2-methylpropanenitrile, Tyrosine-protein kinase BTK | | Authors: | Kuglstatter, A, Wong, A. | | Deposit date: | 2014-09-29 | | Release date: | 2014-12-24 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Finding the perfect spot for fluorine: Improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold.
Bioorg.Med.Chem.Lett., 25, 2015
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4QT1
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3DTW
 | | Crystal structure of the VEGFR2 kinase domain in complex with a benzisoxazole inhibitor | | Descriptor: | 6-chloro-N-pyrimidin-5-yl-3-{[3-(trifluoromethyl)phenyl]amino}-1,2-benzisoxazole-7-carboxamide, Vascular endothelial growth factor receptor 2 | | Authors: | Whittington, D.A, Long, A.M, Rose, P, Gu, Y, Zhao, H. | | Deposit date: | 2008-07-16 | | Release date: | 2008-09-09 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Discovery of amido-benzisoxazoles as potent c-Kit inhibitors.
Bioorg.Med.Chem.Lett., 18, 2008
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4R1Y
 | | Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitor | | Descriptor: | 2-(2-(2-(2-(2-(2-ETHOXYETHOXY)ETHOXY)ETHOXY)ETHOXY)ETHOXY)ETHANOL, 3-(diethylamino)propyl (3-{[5-(3,4-dimethoxyphenyl)-2-oxo-2H-1,3,4-thiadiazin-3(6H)-yl]methyl}phenyl)carbamate, Hepatocyte growth factor receptor | | Authors: | Blaukat, A, Bladt, F, Friese-Hamim, M, Knuehl, C, Fittschen, C, Graedler, U, Meyring, M, Dorsch, D, Stieber, F, Schadt, O. | | Deposit date: | 2014-08-08 | | Release date: | 2015-03-18 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors.
Bioorg.Med.Chem.Lett., 25, 2015
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5CEO
 | | DLK in complex with inhibitor 2-((6-(3,3-difluoropyrrolidin-1-yl)-4-(1-(oxetan-3-yl)piperidin-4-yl)pyridin-2-yl)amino)isonicotinonitrile | | Descriptor: | 2-[[6-[3,3-bis(fluoranyl)pyrrolidin-1-yl]-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrile, Mitogen-activated protein kinase kinase kinase 12 | | Authors: | HARRIS, S.F, YIN, J. | | Deposit date: | 2015-07-07 | | Release date: | 2015-10-14 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (2.28 Å) | | Cite: | Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).
J.Med.Chem., 58, 2015
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5CF5
 | | CRYSTAL STRUCTURE OF JANUS KINASE 2 IN COMPLEX WITH N,N-DICYCLOPROPYL-7-[(DIMETHYL-1,3-THIAZOL-2-YL)AMINO]-10-ETHYL-3-METHYL-3,5,8,10-TETRAAZATRICYCLO[7.3.0.02,6] DODECA-1(9),2(6),4,7,11-PENTAENE-11-CARBOXAMIDE | | Descriptor: | N,N-dicyclopropyl-4-[(4,5-dimethyl-1,3-thiazol-2-yl)amino]-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide, Tyrosine-protein kinase JAK2 | | Authors: | Sack, J.S. | | Deposit date: | 2015-07-08 | | Release date: | 2015-08-26 | | Last modified: | 2015-09-02 | | Method: | X-RAY DIFFRACTION (2.45 Å) | | Cite: | Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.
Acs Med.Chem.Lett., 6, 2015
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3DKC
 | | Structure of MET receptor tyrosine kinase in complex with ATP | | Descriptor: | ADENOSINE-5'-TRIPHOSPHATE, CHLORIDE ION, Hepatocyte growth factor receptor, ... | | Authors: | Hendle, J. | | Deposit date: | 2008-06-24 | | Release date: | 2009-07-07 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (1.52 Å) | | Cite: | SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo.
Mol.Cancer Ther., 8, 2009
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4R3P
 | | Crystal structures of EGFR in complex with Mig6 | | Descriptor: | Epidermal growth factor receptor, peptide from ERBB receptor feedback inhibitor 1 | | Authors: | Park, E, Kim, N, Yi, Z, Cho, A, Kim, K, Ficarro, S.B, Park, A, Park, W.Y, Murray, B, Meyerson, M, Beroukim, R, Marto, J.A, Cho, J, Eck, M.J. | | Deposit date: | 2014-08-17 | | Release date: | 2015-08-12 | | Last modified: | 2015-09-16 | | Method: | X-RAY DIFFRACTION (2.905 Å) | | Cite: | Structure and mechanism of activity-based inhibition of the EGF receptor by Mig6.
Nat.Struct.Mol.Biol., 22, 2015
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4E26
 | | BRAF in complex with an organic inhibitor 7898734 | | Descriptor: | 5-chloro-7-[(R)-furan-2-yl(pyridin-2-ylamino)methyl]quinolin-8-ol, Serine/threonine-protein kinase B-raf | | Authors: | Qin, J, Xie, P, Ventocilla, C, Zhou, G, Vultur, A, Chen, Q, Herlyn, M, Winkler, J, Marmorstein, R. | | Deposit date: | 2012-03-07 | | Release date: | 2012-05-09 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.55 Å) | | Cite: | Identification of a Novel Family of BRAF(V600E) Inhibitors.
J.Med.Chem., 55, 2012
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3DQX
 | | chicken c-Src kinase domain in complex with ATPgS | | Descriptor: | ADENOSINE MONOPHOSPHATE, Proto-oncogene tyrosine-protein kinase Src | | Authors: | Azam, M, Seeliger, M.A, Gray, N, Kuriyan, J, Daley, G.Q. | | Deposit date: | 2008-07-09 | | Release date: | 2008-09-23 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Activation of tyrosine kinases by mutation of the gatekeeper threonine.
Nat.Struct.Mol.Biol., 15, 2008
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4R1V
 | | Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors | | Descriptor: | 3-[1-(3-{5-[(1-methylpiperidin-4-yl)methoxy]pyrimidin-2-yl}benzyl)-6-oxo-1,6-dihydropyridazin-3-yl]benzonitrile, GAMMA-BUTYROLACTONE, Hepatocyte growth factor receptor | | Authors: | Blaukat, A, Bladt, F, Friese-Hamim, M, Knuehl, C, Fittschen, C, Graedler, U, Meyring, M, Dorsch, D, Stieber, F, Schadt, O. | | Deposit date: | 2014-08-07 | | Release date: | 2015-03-18 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (1.2 Å) | | Cite: | Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors.
Bioorg.Med.Chem.Lett., 25, 2015
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4RIO
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